Compound Detail
CHEMBL4585668
BELZUTIFAN 💊 Approved Drug
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💊 Approved Drug
CS(=O)(=O)c1ccc(Oc2cc(F)cc(C#N)c2)c2c1[C@H](O)[C@H](F)[C@@H]2F
Basic Information
| ChEMBL ID | CHEMBL4585668 |
| Name | BELZUTIFAN |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | LOMMPXLFBTZENJ-ZACQAIPSSA-N |
| Therapeutic | ✓ Yes |
3
Targets
8
Activities
2
Assay Types
26
PK Parameters
20
Publications
7
Known Names
9
Indications
1
Mechanisms
Molecular Properties
383.4
MW (Da)
3.29
ALogP
5
HBA
1
HBD
87.4
PSA (Ų)
0.88
QED
0
Ro5 Violations
3
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2021 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Endothelial PAS domain-containing protein 1 inhibitor | INHIBITOR | Endothelial PAS domain-containing protein 1 | ✓ | ✓ |
Indications
Carcinoma, Renal Cell Carcinoma, Renal Cell Carcinoma, Renal Cell Hemangioblastoma Neoplasms Neuroendocrine Tumors von Hippel-Lindau Disease Liver Diseases Renal Insufficiency, Chronic
ATC Classification
L01XX74
belzutifan
Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Level 2: ANTINEOPLASTIC AGENTS
Drug Warnings
Black Box Warning
cardiotoxicity
Black Box Warning
teratogenicity
Activity Summary
EC50 5 meas. best 7.96
IC50 3 meas. best 8.05
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Endothelial PAS domain-containing protein 1 CHEMBL1744522 | IC50 | 8.05 | 8.025 | 9.0 | 2 |
| Endothelial PAS domain-containing protein 1 CHEMBL1744522 | EC50 | 7.96 | 7.865 | 11.0 | 2 |
| Vascular endothelial growth factor A, long form CHEMBL1783 | EC50 | 7.75 | 7.75 | 18.0 | 3 |
| Unchecked CHEMBL612545 | IC50 | 5.05 | 5.05 | 9000.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 2100.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 7100.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 17500.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 25900.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 21000.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 28000.0 | ng.hr.mL-1 | Homo sapiens |
| CL | 21.0 | mL.min-1.kg-1 | Mus musculus |
| CL | 19.0 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 1.3 | mL.min-1.kg-1 | Canis lupus familiaris |
| CL | 3.5 | mL.min-1.kg-1 | Macaca mulatta |
| Cmax | 521.72 | nM | Homo sapiens |
| Cmax | 1304.29 | nM | Homo sapiens |
| Cmax | 3652.02 | nM | Homo sapiens |
| Cmax | 4695.45 | nM | Homo sapiens |
| Cmax | 5217.16 | nM | Homo sapiens |
| Cmax | 7043.17 | nM | Homo sapiens |
| T1/2 | 4.0 | hr | Mus musculus |
| T1/2 | 1.4 | hr | Rattus norvegicus |
| T1/2 | 14.0 | hr | Canis lupus familiaris |
| T1/2 | 9.2 | hr | Macaca mulatta |
| T1/2 | 12.5 | hr | Homo sapiens |
| T1/2 | 18.8 | hr | Homo sapiens |
| T1/2 | 15.4 | hr | Homo sapiens |
| T1/2 | 20.9 | hr | Homo sapiens |
| T1/2 | 12.2 | hr | Homo sapiens |
| T1/2 | 14.1 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine